| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
Demethylmenaquinone methyltransferase (MenG) in Mycobacterium tuberculosis. GSK1733953A inhibits MenG activity, which is responsible for the catalytic methylation of demethylmenaquinone, a key step in the biosynthesis of menaquinone (vitamin K2) in M. tuberculosis.
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|---|---|
| ln Vitro |
GSK1733953A inhibits MenG activity with an IC50 of 2.6 ± 0.6 µM. As a respiratory inhibitor of M. tuberculosis, it disrupts the bacterial respiratory chain by inhibiting menaquinone biosynthesis. The compound is described as the first reported inhibitor of the M. tuberculosis enzyme MenG.
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| ln Vivo |
Specific in vivo activity data for GSK1733953A are not detailed in the available literature. As an inhibitor of M. tuberculosis MenG, it would be expected to have antitubercular activity in vivo. The compound may be utilized in tuberculosis-related research.
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| Enzyme Assay |
In vitro enzyme inhibition assays for GSK1733953A involve measuring the activity of MenG in the presence of varying concentrations of the compound. The enzyme is incubated with its substrate (demethylmenaquinone) and a methyl donor, and the production of menaquinone is quantified. The IC50 value is determined from the dose-response curve.
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| Cell Assay |
In vitro cell-based assays for GSK1733953A assess its antimycobacterial activity against M. tuberculosis cultures. Bacteria are treated with GSK1733953A, and bacterial growth or viability is measured. The minimum inhibitory concentration (MIC) can be determined from dose-response curves. The compound's effects on bacterial respiration can also be assessed.
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| Animal Protocol |
Specific in vivo animal model protocols for GSK1733953A are not described in the available literature. To evaluate its in vivo efficacy, GSK1733953A could be administered to mouse models of tuberculosis infection. Bacterial load in the lungs and other tissues would be measured as endpoints.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for GSK1733953A are not reported in the available literature. As a small molecule inhibitor, its absorption, distribution, metabolism, and excretion properties would need to be characterized for in vivo use. The compound is available as a solid powder.
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| Toxicity/Toxicokinetics |
Specific toxicological data for GSK1733953A are not available. As a research compound targeting M. tuberculosis, its safety profile in mammalian systems has not been comprehensively characterized. Toxicity studies would be required to determine its therapeutic index.
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| References |
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| Additional Infomation |
GSK1733953A is a research tool for studying menaquinone biosynthesis in M. tuberculosis and for developing new antitubercular agents. It is the first reported inhibitor of the M. tuberculosis enzyme MenG. The compound is not an approved therapeutic agent but has potential for tuberculosis research.
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| Molecular Formula |
C21H17CLFNO3
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|---|---|
| Molecular Weight |
385.815988302231
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| Exact Mass |
385.09
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| Elemental Analysis |
C, 65.38; H, 4.44; Cl, 9.19; F, 4.92; N, 3.63; O, 12.44
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| CAS # |
930470-97-6
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| Related CAS # |
930470-97-6 GSK1733953A
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| PubChem CID |
17555992
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| Appearance |
Solid powder
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| LogP |
5.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
486
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RWSCJEILSRMTEH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H17ClFNO3/c1-26-16-7-3-13(4-8-16)18-12-15(6-10-20(18)27-2)24-21(25)17-9-5-14(23)11-19(17)22/h3-12H,1-2H3,(H,24,25)
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| Chemical Name |
2-chloro-4-fluoro-N-[4-methoxy-3-(4-methoxyphenyl)phenyl]benzamide
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| Synonyms |
GSK1733953A; GSK-1733953A; GSK 1733953A; DG70; DG-70; DG 70;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~259.19 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.48 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5919 mL | 12.9594 mL | 25.9188 mL | |
| 5 mM | 0.5184 mL | 2.5919 mL | 5.1838 mL | |
| 10 mM | 0.2592 mL | 1.2959 mL | 2.5919 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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